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Entinostat

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Entinostat
Names
IUPAC name Pyridin-3-ylmethyl N-phenyl]methyl]carbamate
Other names SNDX-275; MS-275
Identifiers
CAS Number
3D model (JSmol)
ECHA InfoCard 100.158.999 Edit this at Wikidata
KEGG
PubChem CID
CompTox Dashboard (EPA)
SMILES
  • C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3
Properties
Chemical formula C21H20N4O3
Molar mass 376.4085
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). checkY verify (what is  ?) Infobox references
Chemical compound

Entinostat, also known as SNDX-275 and MS-275, is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers.

Entinostat inhibits class I HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively.

Clinical trials

There is an ongoing phase II trial studying the effect of entinostat on Hodgkin's lymphoma. It is in other phase II trials for advanced breast cancer (in combination with aromatase inhibitors) and for metastatic lung cancer (in combination with erlotinib).

References

  1. Phase I trial of 5-azacitidine (5AC) and SNDX-275 in advanced lung cancer (NSCLC)
  2. Novel Sulphonylpyrroles as Inhibitors of Hdac S Novel Sulphonylpyrroles
  3. A Phase 2 Multi-Center Study of Entinostat (SNDX-275) in Patient With Relapsed or Refractory Hodgkin's Lymphoma
  4. A Phase 2, Multicenter Study of the Effect of the Addition of SNDX-275 to Continued Aromatase Inhibitor (AI) Therapy in Postmenopausal Women With ER+ Breast Cancer Whose Disease is Progressing
  5. A Phase 2 Exploratory Study of Erlotinib and SNDX-275 in Patients With Non-small Cell Lung Carcinoma Who Are Progressing on Erlotinib


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